Journals and Conferences

Brain Region

Organism

The rapid metabolism of heroin to 6-acetylmorphine and its slower conversion to morphine has led many to believe that heroin and morphine act through the same receptors and that the differences between them are due to their pharmacokinetics. We now present evidence strongly implying that heroin and two potent mu drugs, fentanyl and etonitazine, act through… (More)

Although MOR-1 encodes a mu opioid receptor, its relationship to the pharmacologically defined mu receptor subtypes has been unclear. Antisense mapping now suggests that these subtypes result from alternative splicing of MOR-1. Three oligodeoxynucleotide probes targeting exon 1 and another oligodeoxynucleotide directed against the coding region of exon 4… (More)

There is evidence that angiotensin II has a direct effect on reabsorptive processes of the kidney that are mediated by angiotensin II receptors on the proximal tubules. These receptors have not previously been localized to luminal brush border or basolateral membranes. The present study is the first to characterize the angiotensin II receptor of rat renal… (More)

Morphine-6beta-glucuronide (M6G) is a potent morphine metabolite. In an effort to further explore its mechanisms of action, we synthesized 3H-M6G of high specific activity and examined its binding. Although its affinity toward traditional mu receptors is similar to morphine in binding assays in brain and in Chinese hamster ovary cells stably transfected… (More)

Long-term potentiation (LTP) can be induced in the Schaffer collateral-->CA1 synapse of hippocampus by stimulation in the theta frequency range (5-12 Hz), an effect that depends on activation of the cAMP pathway. We investigated the mechanisms of the cAMP contribution to this form of LTP in the rat hippocampal slice preparation. theta pulse stimulation… (More)

Recent work has suggested that heroin and morphine-6beta-glucuronide (M6G) both act through a novel mu opioid receptor subtype distinct from those mediating morphine's actions. This very high affinity 3H-M6G site is selectively competed by 3-methoxynaltrexone. In vivo, 3-methoxynaltrexone (2.5 ng, i.c.v.) selectively antagonizes the analgesic actions of… (More)

Naloxone benzoylhydrazone (NalBzoH) is a potent mu antagonist in vivo. In a cell line stably transfected with MOR-1 (CHO/MOR-1), NalBzoH also was an antagonist when examined in adenylyl cyclase studies. In binding studies, it displayed high affinity for the mu receptor, confirming its earlier characterization in brain membranes. In competition studies under… (More)